中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology

文献类型:期刊论文

作者Suo, Yanrui1,2; Xu, Min3; Sun, Meimei1; Lu, Weiwei1; Wang, Xuan1; Lu, Xiaojie1,2
刊名ORGANIC LETTERS
出版日期2022-12-07
页码5
ISSN号1523-7060
DOI10.1021/acs.orglett.2c03759
通讯作者Wang, Xuan(wangxuan2@simm.ac.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn)
英文摘要Indane and isoindoline are attractive bicyclic systems in biologically active compounds but are rarely reported in DNA-encoded libraries. In this paper, we reported an efficient and versatile approach for assembling indane and isoindoline scaffolds via a ruthenium-catalyzed [2 + 2 + 2] cyclotrimerization reaction. This method exhibits a broad substrate scope and has been successfully applied to construct a 53K-membered DNA-encoded library (DEL). In order to test its application, we carried out a preliminary selection of this DEL against Aurora A protein and identified a hit compound with 9.3 mu M inhibition activity.
WOS关键词CHEMISTRY ; DANOPREVIR ; DISCOVERY ; SELECTION ; DESIGN
资助项目Shanghai Municipal Science and Technology Major Project ; [NSFC-91953203] ; [NSFC-21877117] ; [NSFC-21907103]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000893455600001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/304324]  
专题新药研究国家重点实验室
通讯作者Wang, Xuan; Lu, Xiaojie
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
推荐引用方式
GB/T 7714
Suo, Yanrui,Xu, Min,Sun, Meimei,et al. Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology[J]. ORGANIC LETTERS,2022:5.
APA Suo, Yanrui,Xu, Min,Sun, Meimei,Lu, Weiwei,Wang, Xuan,&Lu, Xiaojie.(2022).Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology.ORGANIC LETTERS,5.
MLA Suo, Yanrui,et al."Ruthenium-Mediated [2+2+2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology".ORGANIC LETTERS (2022):5.

入库方式: OAI收割

来源:上海药物研究所

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